Analogs a drug vildagliptin * metformin * (vildagliptin * metformin *)

Oral hypoglycemic mankhwala. Vildagliptin - nthumwi ya kalasi ya zopititsa patsogolo zomwe zimapangidwira pancreas, mosankha zimalepheretsa pulotidyl peptidase-4 (DPP-4) ya enzyme. Kulepheretsa mwachangu komanso kwathunthu kwa ntchito ya DPP-4 (> 90%) kumayambitsa kuwonjezeka kwa kubisa komanso kokhala ndi chakudya komwe kumapangitsa mtundu wa 1 glucagon-peptide (GLP-1) ndi glucose-wodalira insulinotropic polypeptide (HIP) kuchokera kumatumbo kulowa kutsekemera kwazinthu tsiku lonse.

Kuchulukitsa kuzungulira kwa GLP-1 ndi HIP, vildagliptin kumapangitsa kuwonjezeka kwa chidwi cha pancreatic β-cell ku glucose, zomwe zimabweretsa kusintha kwa secretion wa glucose-based insulin.

Mukamagwiritsa ntchito vildagliptin pa mlingo wa 50-100 mg wa patsiku kwa odwala omwe ali ndi matenda a shuga 2, kusintha kwa ntchito ya kapamba kumadziwika. Kukula kwa magwiridwe antchito a cells-cell kumadalira kuchuluka kwa kuwonongeka kwawo koyambirira, choncho mwa anthu omwe alibe matenda a shuga mellitus (omwe ali ndi shuga wa m'magazi), vildagliptin simalimbikitsa kutulutsa kwa insulin komanso sikuchepetsa shuga.

Mwakulitsa kuchuluka kwa mawonekedwe amkati mwa GLP-1, vildagliptin kumawonjezera chidwi cha maselo a α-glucose, zomwe zimapangitsa kuti pakhale kusintha kwamalamulo a shuga a glucagon. Kutsika kwa glucagon ochulukirapo panthawi ya chakudya, kumayambitsa kuchepa kwa insulin.

Kuwonjezeka kwa kuchuluka kwa insulin / glucagon poyang'ana kumbuyo kwa hyperglycemia, chifukwa cha kuchuluka kwa kuchuluka kwa GLP-1 ndi HIP, kumayambitsa kuchepa kwa kupanga kwa chiwindi ndi chiwindi chonse munthawi ya chakudya ndikatha kudya, zomwe zimayambitsa kuchepa kwa kuchuluka kwa shuga m'magazi am'magazi.

Kuphatikiza apo, motsutsana ndi magwiritsidwe ntchito a vildagliptin, kuchepa kwa milomo ya lipids m'magazi amwazi kumadziwika, komabe, izi sizikugwirizana ndi zomwe zimachitika pa GLP-1 kapena HIP komanso kusintha kwa ntchito ya pancreatic β-cell.

Amadziwika kuti kuwonjezeka kwa GLP-1 kumatha kuchepetsa m'mimba, koma izi sizikuwoneka ndi kugwiritsa ntchito vildagliptin.

Mukamagwiritsa ntchito vildagliptin mu 5795 odwala omwe ali ndi mtundu wa 2 shuga mellitus kwa masabata 12 mpaka 52 monga monotherapy kapena osakanikirana ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, kapena insulin, kuchepa kwakukulu kwakanthawi kwakanthawi kwa kuchuluka kwa glycated hemoglobin (HbA1c) komanso kusala glucose.

Pamene kuphatikiza kwa vildagliptin ndi metformin kunagwiritsidwa ntchito ngati chithandizo choyambirira cha odwala omwe ali ndi matenda a shuga 2, kuchepa kwa HbA1c komanso kulemera kwa thupi kumawonedwa pakadutsa masabata 24 poyerekeza ndi monotherapy ndi mankhwalawa. Milandu ya hypoglycemia inali yochepa kwambiri m'magulu onse awiri ochiritsira.

Mu kafukufuku wazachipatala ogwiritsa ntchito vildagliptin pa mlingo wa 50 mg kamodzi patsiku kwa miyezi 6 kwa odwala omwe ali ndi matenda a shuga 2 kuphatikiza ndi kuchepa kwapakati kwa aimpso (GFR> 30 mpaka 1500 mg) kuphatikiza ndi glimepiride (> 4 mg /) Poyesedwa pachipatala, kuchuluka kwa HbA1c pang'onopang'ono kunatsika ndi 0.76% (basement - avareji ya 8.8%).

Pharmacokinetics

Vildagliptin imatengedwa mwachangu ndi kumeza ndi bioavailability yokwanira 85%. Mothandizidwa ndi kuchuluka kwa mankhwalawa, kuchuluka kwa mankhwala a Cmax a vildagliptin mu plasma ndi AUC kuli pafupifupi kukuwonjezereka kwa kuchuluka kwa mankhwalawa.

Pambuyo pakulowetsa pamimba yopanda kanthu, nthawi yofikira Cmax ya vildagliptin m'madzi am'magazi ndi 1 h 45 min. Ndi kudya kwa nthawi yomweyo, kuchuluka kwa mankhwalawa kumacheperachepera: pali kuchepa kwa Cmax ndi 19% ndikuwonjezereka kwa nthawi yomwe imafika maola 2 mphindi 30. Komabe, kudya sikumakhudza kuchuluka kwa mayamwidwe ndi AUC.

Kumangiriza kwa vildagliptin kuma protein a plasma ndikotsika (9.3%). Mankhwalawa amagawidwa chimodzimodzi pakati pa plasma ndi maselo ofiira amwazi. Kugawa kwa vildagliptin kumachitika mopitilira muyeso, Vd yofanana pambuyo povomerezeka ndi iv.

Biotransfform ndiye njira yayikulu yodziwitsira ya vildagliptin. Mu thupi la munthu, 69% ya mlingo wa mankhwalawo amasandulika. Metabolite yayikulu - lay151 (57% ya mlingo) imagwira ntchito pamankhwala ndipo ndi chida cha hydrolysis cha gawo la cyano. Pafupifupi 4% ya mankhwala omwe amapezeka amide hydrolysis.

M'maphunziro oyesera, zotsatira zabwino za DPP-4 pa hydrolysis yamankhwala zimadziwika. Vildagliptin sichimaphatikizidwa ndi gawo la cytochrome P450 isoenzymes. Vildagliptin si gawo lapansi la CYP450 isoenzymes, sichikuletsa ndipo sichilowetsa cytochrome P450 isoenzymes.

Pambuyo pakulowetsa mankhwalawa, pafupifupi 85% ya mankhwalawa imachotsedwa impso ndi 15% kudzera m'matumbo, impso ya vildagliptin yosasinthika ndi 23%. T1 / 2 pambuyo pakumwa pakamwa ndi pafupifupi maola atatu, mosasamala kanthu.

Gender, index misa, ndi mafuko sizikhudzanso pharmacokinetics ya vildagliptin.

Zisonyezero zamankhwala GALVUS

Type 2 matenda a shuga:

• monga monotherapy kuphatikizapo mankhwala othandizira ndi masewera olimbitsa thupi,
• kuphatikiza ndi metformin ngati mankhwala oyamba ndimankhwala osakwanira othandizira kudya komanso kuchita masewera olimbitsa thupi,
• monga gawo limodzi la magawo awiri ophatikizira mankhwala a metformin, zotumphukira za sulfonylurea, thiazolidinedione kapena insulini popewa kugwiritsa ntchito mankhwala osokoneza bongo, kuchita masewera olimbitsa thupi komanso monotherapy ndi mankhwalawa.
• Monga mbali ya mankhwala ophatikiza patatu: kuphatikiza ndi mankhwala a sulfonylurea ndi metformin odwala omwe kale amathandizidwa ndi zotumphukira zochokera ku sulfonylurea ndi metformin motsutsana ndi maziko azakudya ndi masewera olimbitsa thupi komanso omwe sanakwanitse kuwongolera glycemic yoyenera,
• Monga mbali ya mankhwala ophatikiza patatu: kuphatikiza insulin ndi metformin mwa odwala omwe kale adalandira insulin ndi metformin pazakudya ndi masewera olimbitsa thupi omwe sanakwanitse kuyendetsa bwino glycemic.

Mlingo

Galvus amatengedwa pakamwa mosasamala kanthu za chakudya.

Mlingo wa mankhwalawa wa mankhwalawa uyenera kusankhidwa payekha kutengera momwe umagwirira ntchito komanso kulolera.

Mlingo wovomerezeka wa mankhwalawa nthawi ya monotherapy kapena ngati gawo limodzi la mankhwala ophatikizika ndi metformin, thiazolidinedione kapena insulin (osakanikirana ndi metformin kapena opanda metformin) ndi 50 mg kapena 100 mg patsiku. Odwala omwe ali ndi mtundu wovuta kwambiri wa matenda a shuga a 2 omwe amalandiridwa ndi insulin, Galvus amalimbikitsidwa pa 100 mg tsiku lililonse.

Mlingo wovomerezeka wa Galvus monga gawo limodzi la mankhwala ophatikiza katatu (vildagliptin + sulfonylurea derivatives + metformin) ndi 100 mg patsiku.

Mlingo wa 50 mg patsiku uyenera kutumikiridwa mu 1 piritsi. Mlingo wa 100 mg patsiku uyenera kutumikiridwa 50 mg kawiri pa tsiku m'mawa komanso madzulo.

Ikagwiritsidwa ntchito ngati gawo limodzi la magawo awiri ophatikizika ndi mankhwala a sulfonylurea, mlingo woyenera wa Galvus ndi 50 mg 1 nthawi patsiku m'mawa. Mankhwala akaphatikizana ndi mankhwala a sulfonylurea, mphamvu ya mankhwala pa mlingo wa 100 mg patsiku inali yofanana ndi ya 50 mg patsiku. Ndi osakwanira kachipatala motsutsana ndi maziko ogwiritsa ntchito mlingo wapamwamba wa tsiku lililonse wa 100 mg, kuti muthane ndi vuto la glycemia, mankhwala ena a hypoglycemic ndiwothekanso: metformin, zotumphukira za sulfonylurea, thiazolidinedione kapena insulin.

Odwala omwe ali ndi vuto laimpso wofatsa komanso kwa chiwindi, kusintha kwa mlingo sikofunikira. Odwala omwe ali ndi pakati kapena matenda opatsika aimpso (kuphatikizapo matenda omwe amalephera kupweteka aimpso), mankhwalawa ayenera kugwiritsidwa ntchito pa mlingo wa 50 mg kamodzi patsiku.

Odwala okalamba (zaka 65), palibe kusintha kwa mtundu wa Galvus kofunikira.

Popeza palibe chidziwitso pakugwiritsa ntchito mankhwalawa kwa ana ndi achinyamata osakwana zaka 18, sikulimbikitsidwa kugwiritsa ntchito mankhwalawa m'gulu la odwala.

Zotsatira zoyipa

Mukamagwiritsa ntchito Galvus ngati monotherapy kapena kuphatikiza mankhwala ena, zovuta zambiri sizinali zofatsa, zosakhalitsa, ndipo sizinafune kusiya chithandizo. Palibe kulumikizana komwe kunapezeka pakati pa zochita zazosiyana ndi msinkhu, jenda, fuko, nthawi yogwiritsira ntchito, kapena mtundu wa dosing.

Zomwe zimachitika ndi angioedema pa chithandizo ndi Galvus anali> 1/10 000, 3 × VGN) anali 0,2% kapena 0,3%, motero (poyerekeza ndi 0,2% pagulu lolamulira). Kuchulukana kwa ntchito ya ma enzymes a chiwindi nthawi zambiri kunali asymptomatic, sikunapite patsogolo, ndipo sikunayendetsedwe ndi kusintha kwa cholestatic kapena jaundice.

Kutsimikiza kwamafotokozedwe azovuta: nthawi zambiri (> 1/10), nthawi zambiri (> 1/100, 1/1000, 1/10 000, 2,5 kuchulukirapo kuposa VGN).

Popeza luso logwiritsa ntchito Galvus odwala omwe ali ndi vuto loti-a hemomyalysis ndilochepa, tikulimbikitsidwa kuti mankhwalawa adapangidwe mosamala mu gulu ili la odwala.

Kugwiritsa ntchito mankhwala GALVUS pa mimba ndi mkaka wa m`mawere

Palibe deta yokwanira yogwiritsidwa ntchito ndi Galvus mwa amayi apakati, chifukwa chake mankhwalawa sayenera kugwiritsidwa ntchito panthawi yoyembekezera. Milandu ya vuto logaya shuga mwa amayi apakati, pamakhala chiwopsezo chodzala ndi vuto lobadwa nalo, komanso kufalikira kwamatenda a kubadwa kwa neonatal.

Mu kafukufuku woyesera, atalembedwa muyezo Mlingo 200% kuposa momwe analimbikitsira, mankhwalawa sanayambitse chonde ndikukula koyambirira kwa mwana wosabadwayo ndipo sanatanthauze mwana wosabadwayo.

Popeza sizikudziwika ngati vildagliptin yachotsedwa mkaka waumunthu, Galvus sayenera kugwiritsidwa ntchito pa mkanda wa mkaka.

Malangizo apadera

Popeza nthawi zina vildagliptin imagwiritsidwa ntchito, kuwonjezeka kwa zochitika za aminotransferases (nthawi zambiri popanda mawonetseredwe azachipatala) kunadziwika, kusanachitike kwa Galvus, komanso pafupipafupi mchaka choyamba cha mankhwala ndi mankhwala (nthawi 1 m'miyezi itatu), tikulimbikitsidwa kudziwa magawo awiri am'magazi a ntchito ya chiwindi. Wodwala akakhala ndi zochita zambiri za aminotransferases, zotsatira zake ziyenera kutsimikiziridwa ndi kafukufuku wachiwiri, kenako azindikire magawo a ziwindi za chiwindi ntchito kufikira atasintha. Ngati zochitika za AST kapena ALT ndizokwera katatu kuposa VGN (monga zimatsimikiziridwa ndi maphunziro obwerezedwa), tikulimbikitsidwa kuletsa mankhwalawo.

Ndi chitukuko cha jaundice kapena zizindikiro zina zamagulu operewera a chiwindi pakhungu la Galvus, mankhwalawa ayenera kuyimitsidwa nthawi yomweyo. Pambuyo pakuwonetsa zizindikiro za ntchito ya chiwindi, chithandizo cha mankhwala sichitha kuyambiranso.

Ngati ndi kotheka, mankhwala a insulin Galvus amangogwiritsidwa ntchito limodzi ndi insulin. Mankhwala sayenera kugwiritsidwa ntchito kwa odwala omwe ali ndi matenda a shuga 1 kapena mankhwalawa a matenda ashuga a ketoacidosis.

Bongo

Galvus imalekeredwa bwino ngati iperekedwa pa mlingo wa mpaka 200 mg patsiku.

Zizindikiro: mukamagwiritsa ntchito mankhwalawa 400 mg patsiku, kupweteka kwa minofu kumatha kuchitika, kawirikawiri, mapapo komanso kufupika kwa paresthesia, kutentha thupi, kutupa ndi kuchuluka kwapang'onopang'ono kwa ndende ya lipase (2 times kuposa VGN). Ndi kuwonjezeka kwa mlingo wa Galvus mpaka 600 mg patsiku, kukulitsa edema ya malekezero okhala ndi paresthesias ndi kuwonjezeka kwa kuchuluka kwa CPK, ALT, protein-m-yogwira komanso myoglobin ndizotheka. Zizindikiro zonse za mankhwala osokoneza bongo komanso kusintha kwa magawo a ma laboratite amatha pambuyo pakutha kwa mankhwalawa.

Chithandizo: Kuchotsa mankhwalawa m'thupi kudzera mu dialysis ndikosatheka. Komabe, hydrolytic metabolite yayikulu ya vildagliptin (lay151) imatha kuchotsedwa m'thupi ndi hemodialysis.

Kuyanjana kwa mankhwala osokoneza bongo

Galvus ali ndi mwayi wotsika wolumikizana ndi mankhwala.

Popeza Galvus si gawo laling'ono la ma enzymes a cytochrome P450, komanso sikulepheretsa kapena kuyambitsa ma enzyme awa, kuyanjana kwa Galvus ndi mankhwala omwe ali apansi, zoletsa, kapena inducers a P450 sizokayikitsa. Pogwiritsa ntchito nthawi yomweyo vildagliptin sikukhudzanso kuchuluka kwa kagayidwe kazakudya kamene kamakhala mu ma enzyme: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 ndi CYP3A4 / 5.

Matenda amakhudzana kwambiri ndi mankhwalawa Galvus ndi mankhwalawa omwe amagwiritsidwa ntchito kwambiri pochizira matenda amishuga 2 mellitus (glibenclamide, pioglitazone, metformin) kapena wokhala ndi masanjidwe ocheperako achire (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin).

Kufotokozera za mankhwalawa

Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) - Pharmacodynamics

Kapangidwe ka mankhwala Vildagliptin * + Metformin * (Vildagliptin * + Metformin *) akuphatikiza ma cell awiri a hypoglycemic omwe ali ndi njira zosiyanasiyana zochitira: vildagliptin, omwe ali mgulu la dipeptidyl peptidase-4 inhibitors (DPP-4), ndi metformin (mwa mtundu wa hydrochloride), wamkulu wa hydrochloride) . Kuphatikizidwa kwa zinthuzi kumakupatsani mwayi wolamulira kuchuluka kwa shuga m'magazi a 2 omwe ali ndi matenda a shuga a 24.

Vildagliptin, nthumwi ya kalasi ya zopititsa patsogolo ziwiya zapachiberekero, mosamala zimalepheretsa enzyme DPP-4, yomwe imawononga mtundu wa 1 glucagon ngati peptide (GLP-1) ndi insulinotropic polypeptide (HIP) yodalira glucose. Metformin imachepetsa kupanga shuga ndi chiwindi, imachepetsa kuyamwa kwa glucose m'matumbo ndikuchepetsa kukana kwa insulin polimbikitsa kutulutsa ndi kugwiritsa ntchito shuga mwa zotumphukira zake.

Metformin imathandizira kuphatikizika kwa glycogen synthetase pochita glycogen synthetase ndipo imakulitsa mayendedwe a glucose ndi mapuloteni ena amtundu wa glucose transporter (GLUT-1 ndi GLUT-4).

Kulepheretsa mwachangu komanso kwathunthu kwa ntchito ya DPP-4 pambuyo pa vildagliptin kumayambitsa kuwonjezeka kwa zonse zoyambira komanso zotsitsimutsa chakudya za GLP-1 ndi HIP kuchokera m'matumbo kulowa kutsekemera kwatsiku lonse.

Kuchulukitsa kuchuluka kwa GLP-1 ndi HIP, vildagliptin kumapangitsa kuwonjezeka kwa chidwi cha pancreatic β-cell ku glucose, zomwe zimabweretsa kusintha kwa secretion wa glucose-based insulin. Kuchulukitsa kwa magwiridwe antchito a β-cell kumadalira kuchuluka kwa kuwonongeka kwawo koyamba, choncho mwa anthu opanda shuga - omwe amakhala ndi shuga m'magazi am'magazi), vildagliptin simalimbikitsa kutulutsa kwa insulin komanso sikuchepetsa kuchuluka kwa shuga.

Mwakulitsa kuchuluka kwa mawonekedwe amkati mwa GLP-1, vildagliptin kumawonjezera chidwi cha β-cell ku glucose, komwe kumabweretsa kusintha kwa kayendedwe ka glucose komwe kamadalira shuga. Kutsika kwa kuchuluka kwa glucagon okwanira mutatha kudya, kumapangitsa kuchepa kwa insulin.

Kuwonjezeka kwa kuchuluka kwa insulin / glucagon motsutsana ndi maziko a hyperglycemia, chifukwa cha kuchuluka kwa kuchuluka kwa GLP-1 ndi HIP, kumayambitsa kuchepa kwa kupanga kwa shuga ndi chiwindi nthawi ya chakudya komanso pambuyo pake, zomwe zimayambitsa kuchepa kwa kuchuluka kwa shuga m'magazi am'magazi.

Kuphatikiza apo, motsutsana ndi kagwiritsidwe ntchito ka vildagliptin, kuchepa kwa kuchuluka kwa lipids m'madzi am'magazi pambuyo podyedwa, komabe, izi sizikugwirizana ndi zomwe zimachitika pa GLP-1 kapena HIP komanso kusintha kwa magwiridwe antchito a cell pancreatic islet. Amadziwika kuti kuwonjezeka kwa kuchuluka kwa GLP-1 kungapangitse kuti m'mimba muchepetse, komabe, motsutsana ndi maziko ogwiritsa ntchito vildagliptin, izi sizikuwoneka.

Mukamagwiritsa ntchito vildagliptin mu 5759 odwala omwe ali ndi mtundu wa 2 shuga mellitus wa masabata 52 mu monotherapy kapena osakanikirana ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, kapena insulin, kuchepa kwakukulu kwakanthawi kwakanthawi kwa kuchuluka kwa glycated hemoglobin (HbA1c) komanso kusala shuga wamagazi.

Metformin imathandizira kulolerana kwa glucose mwa odwala omwe ali ndi matenda a shuga 2 mwakuchepetsa kuchuluka kwa glucose nthawi yoyamba komanso isanachitike.

Mosiyana ndi mankhwala a sulfonylurea, metformin sayambitsa hypoglycemia kwa odwala omwe ali ndi matenda a shuga 2 kapena anthu athanzi (kupatula milandu yapadera). Mankhwalawa ndi mankhwalawa sikuti kumayambitsa kukula kwa hyperinsulinemia. Pogwiritsa ntchito metformin, insulin katulutsidwe sikusintha, pamene kuchuluka kwa insulin m'mimba yopanda kanthu komanso masana kumatha kuchepa.

Pogwiritsa ntchito metformin, phindu pa kagayidwe ka lipoproteins limadziwika: kuchepa kwa kuchuluka kwa cholesterol, cholesterol yotsika milomo ya lipoproteins ndi triglycerides, osagwirizana ndi mphamvu ya mankhwalawa pakupezeka kwa shuga m'magazi am'magazi.

Mukamagwiritsa ntchito mankhwala ophatikizira ndi vildagliptin ndi metformin mu Mlingo wa tsiku ndi tsiku wa 1,500-3,000 mg wa metformin ndi 50 mg wa vildagliptin 2 nthawi / tsiku kwa chaka chimodzi, kuchepa kwakukulu kwa kuchuluka kwa shuga m'magazi kunawonedwa (kutsimikizika ndi kuchepa kwa HbA1c) komanso kuchuluka kwa odwala omwe ali ndi kuchepa. Kuyika kwa HbA1c sikunali kochepera 0.6-0.7% (poyerekeza ndi gulu la odwala omwe akupitiliza kulandira metformin yokha).

Odwala omwe amalandila vildagliptin ndi metformin, kusintha kwakukulu pa kulemera kwamunthu poyerekeza ndi koyambirira sikunawonedwe. Masabata 24 atayamba chithandizo, m'magulu a odwala omwe amalandila vildagliptin osakanikirana ndi metformin, panali kuchepa kwa magazi a systolic ndi diastolic kwa odwala omwe ali ndi matenda oopsa.

Pamene kuphatikiza kwa vildagliptin ndi metformin kunagwiritsidwa ntchito ngati chithandizo choyambirira cha odwala omwe ali ndi mtundu wa 2 matenda a shuga, kuchepa kwa mlingo wa HbA1c kumawonedwa pakadutsa masabata 24 poyerekeza ndi monotherapy ndi mankhwalawa. Milandu ya hypoglycemia inali yochepa kwambiri m'magulu onse awiri ochiritsira.

Mukamagwiritsa ntchito vildagliptin (50 mg 2 nthawi / tsiku) nthawi yomweyo ndi / popanda metformin osakanikirana ndi insulin (pafupifupi mlingo wa 41 PIECES) mwa odwala omwe ali pachiyeso chachipatala, chizindikiro cha HbA1c chinawerengeka kwambiri ndi 0.72% (chizindikiro choyambirira, pafupifupi 8,8%). Chiwopsezo cha hypoglycemia mwa odwala omwe amathandizidwa chinali chofanana ndi kuchuluka kwa hypoglycemia mu gulu la placebo.

Mukamagwiritsa ntchito vildagliptin (50 mg 2 nthawi / tsiku) nthawi yomweyo ndi metformin (> 1500 mg) osakanikirana ndi glimepiride (> 4 mg patsiku) mwa odwala omwe ali pachiyeso cham'chipatala, chiwonetsero cha HbA1c chiwerengero chatsika kwambiri ndi 0.76% (kuchokera pafupifupi 8.8%) .

Mndandanda wazofananira

Fomu ya Mlingo:

mapiritsi okhala ndi filimu

Piritsi limodzi lachifundo 1
ntchito: vildagliptin 50.0 mg ndi metformin hydrochloride 500.0 mg, 850.0 mg kapena 1000.0 mg,
zokopa: hyprolose, magnesium stearate, hypromellose, titanium dioxide (E 171), macrogol 4000, talc, iron iron oxide (E 172).
Mapiritsi a 50 mg + 500 mg ophatikizidwa ndi mafilimu amaphatikizanso ndi iron oxide ofiira (E172)

Kufotokozera:
Mapiritsi okhala ndi mafilimu. 50 mg + 500 mg: mapiritsi osalala okhala ndi mbali zokutidwa, yokutidwa ndi kanema, wachikasu wopepuka komanso wamtambo wa pinki. Kumbali ina ya cholembapo ndikulemba "NVR", mbali inayo - "LLO".
Mapiritsi okhala ndi mafilimu, 50 mg + 850 mg: mapiritsi osalala okhala ndi mbali zokutidwa, utoto wokutira wamafuta ndi utoto wonyezimira. Kumbali ina ya cholembapo ndikulemba "NVR", mbali inayo - "SEH".
Mapiritsi okhala ndi mafilimu. 50 mg + 1000 mg: mapiritsi osalala okhala ndi mbali zomata, film-yokutira yakuda yachikasu ndi utoto wamafuta. Kumbali ina ya phale kulembapo "NVR", mbali inayo ndi "FLO".

Zotsatira za kugwiritsa ntchito mankhwala GALVUS MET

• Kulephera kwa impso kapena kuwonongeka kwa impso: ndi mulingo wa serum creatinine> 1.5 mg% (> 135 μmol / L) kwa amuna ndi> 1.4 mg% (> 110 μmol / L) kwa amayi,
• zovuta pachimake ndi chiwopsezo cha aimpso kukanika: kuchepa magazi (ndi kutsegula m'mimba, kusanza), kutentha thupi, matenda opatsirana, mikhalidwe ya hypoxia (mantha, sepsis, matenda a impso, matenda a bronchopulmonary),
• kukomoka mtima komanso kupsinjika kwa mtima, kupweteka kwa mtima kwambiri, kulephera kwamtima ndi mantha (mantha),
• kulephera kupuma
• chiwindi ntchito,
• pachimake kapena matenda metabolic acidosis (kuphatikizapo matenda ashuga a ketoacidosis osakanikirana kapena wopanda chikomokere). Matenda ashuga ketoacidosis ayenera kuwongoleredwa ndi insulin mankhwala,
• lactic acidosis (kuphatikizapo mbiri),
• Mankhwalawa sanalembedwe masiku awiri asanachitike opaleshoni, radioisotope, maphunziro a x-ray ndikuyambitsa kwa othandizira ndipo pakatha masiku awiri atachitidwa,
• mimba
• kuyamwa
• mtundu 1 shuga
• uchidakwa wambiri, chakumwa chakumwa choledzeretsa,
• kutsatira zakudya zopatsa mphamvu (zosakwana 1000 kcal / tsiku),
• ana ochepera zaka 18 (mphamvu ndi chitetezo chogwiritsa ntchito sizinakhazikitsidwe),
• Hypersensitivity to vildagliptin kapena metformin kapena chilichonse cha mankhwala.

Popeza odwala omwe ali ndi vuto la chiwindi ntchito nthawi zina, lactic acidosis adadziwika, yomwe mwina ndi imodzi mwazotsatira zoyipa za metformin, Galvus Met sayenera kugwiritsidwa ntchito mwa odwala omwe ali ndi matenda a chiwindi kapena magawo ophatikizika a hepatic biochemical.

Mosamala, tikulimbikitsidwa kugwiritsa ntchito mankhwala okhala ndi metformin mwa odwala opitirira zaka 60, komanso pochita ntchito yayitali chifukwa chakuwopsa kwa lactic acidosis.

Mankhwala

Mankhwala
Kapangidwe ka Gal Gal Met kamakhala ndi othandizira awiri a hypoglycemic omwe ali ndi njira zosiyanasiyana zochitira: vildagliptin, omwe ali mgulu la dipeptidyl peptidase-4 zoletsa, ndi metformin (mu mawonekedwe a hydrochloride), woimira kalasi yayikulu. Kuphatikizidwa kwa zinthuzi kumakupatsani mwayi wowongolera kuchuluka kwa shuga m'magazi omwe ali ndi matenda a shuga a 2 pasanathe maola 24.

Vildagliptia
Vildagliptin, membala wa gulu la othandizira makina ogwiritsira ntchito pancreatic, mosamala amaletsa enzyme dipeptidyl peptidase-4 (DPP-4), yomwe imawononga mtundu wa 1 glucagon-peptide (GLP-1) ndi insulinotropic polypeptide (HIP) yodalira glucose.
Kuletsa mwachangu komanso kwathunthu ntchito za DPP-4 kumayambitsa kuwonjezeka kwa zonse zoyambira komanso zotsitsimutsa chakudya za GLP-1 ndi HIP kuchokera m'matumbo kulowa kutsekeka kwadongosolo tsiku lonse.
Mwakuwonjezera milingo ya GLP-1 ndi HIP, vildagliptin imayambitsa kukhudzika kwa maselo a pancreatic to-glucose, zomwe zimabweretsa kusintha kwa secretion ya shuga. Kukula kwa magwiridwe antchito a p-maselo kumadalira kuchuluka kwa kuwonongeka kwawo koyamba, choncho mwa anthu omwe alibe matenda a shuga mellitus (omwe ali ndi shuga wa m'magazi), vildagliptin simalimbikitsa kutulutsa kwa insulin komanso sikuchepetsa shuga.
Mwa kuwonjezera milingo ya amkati mwa GLP-1, vildagliptin imawonjezera chidwi cha maselo a клеток ku glucose, zomwe zimabweretsa kusintha kwa kayendedwe ka glucose komwe kamadalira glucagon. Kutsika kwa glucagon ochulukirapo panthawi ya chakudya, kumayambitsa kuchepa kwa insulin.
Kuwonjezeka kwa kuchuluka kwa insulin / glucagon motsutsana ndi maziko a hyperglycemia, chifukwa cha kuchuluka kwa GLP-1 ndi HIP, kumayambitsa kuchepa kwa kupanga kwa shuga ndi chiwindi nthawi yakudya komanso itatha, zomwe zimabweretsa kuchepa kwa shuga m'magazi.
Kuphatikiza apo, motsutsana ndi kagwiritsidwe ntchito ka vildagliptin, kuchepa kwa milomo ya lipids m'madzi am'magazi pambuyo podyedwa, komabe, izi sizikugwirizana ndi zomwe zimachitika pa GLP-1 kapena HIP komanso kusintha kwa magwiridwe antchito a cell pancreatic.
Amadziwika kuti kuwonjezeka kwa GLP-1 kumatha kuchepetsa m'mimba, koma izi sizikuwoneka ndi kugwiritsa ntchito vildagliptin. Mukamagwiritsa ntchito vildagliptin mu 5759 odwala omwe ali ndi mtundu wa 2 shuga mellitus wa masabata 52 monga monotherapy kapena osakanikirana ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, kapena insulin, kuchepa kwakukulu kwakanthawi kwakanthawi kwa kuchuluka kwa glycated hemoglobin (HbA_1c) komanso kusala magazi.

Metformin
Metformin imathandizira kulolerana kwa glucose mwa odwala omwe ali ndi matenda a shuga 2 mwakuchepetsa shuga m'magazi asanafike komanso atatha kudya. Metformin imachepetsa kupanga shuga ndi chiwindi, imachepetsa kuyamwa kwa glucose m'matumbo ndikuchepetsa kukana kwa insulin polimbikitsa kutulutsa ndi kugwiritsa ntchito shuga mwa zotumphukira zake. Mosiyana ndi mankhwala a sulfanylurea, metformin sayambitsa hypoglycemia mwa odwala omwe ali ndi matenda a shuga 2 kapena m'mawu athanzi (kupatula milandu yapadera). Mankhwalawa ndi mankhwalawa sikuti kumayambitsa kukula kwa hyperinsulinemia. Pogwiritsa ntchito metformin, insulin katulutsidwe sikasintha, pomwe ma insulin plasma pamimba yopanda kanthu komanso masana amatha kuchepa.
Metformin imathandizira kuphatikizika kwa glycogen synthesis mwa glycogen synthase ndikukulitsa kutulutsa kwa glucose ndi mapuloteni ena amtundu wa glucose transporter (GLUT-1 ndi GLUT-4).
Metformin ikagwiritsidwa ntchito, zotsatira zopindulitsa kagayidwe ka lipoproteins zimadziwika: kuchepa kwa kuchuluka kwa cholesterol, otsika kachulukidwe lipoprotein cholesterol ndi triglycerides, osagwirizana ndi mphamvu ya mankhwalawa m'magazi a glucose.

Vildagliptin + Metformin
Mukamagwiritsa ntchito mankhwala othandizira a vildagliptin / metformin mu Mlingo wa tsiku ndi tsiku wa 1500 - 3000 mg wa metformin ndi 50 mg wa vildagliptin 1 chaka, kuchepa kwakukulu kwa kuchuluka kwa shuga m'magazi kunawonedwa (kutsimikiziridwa ndi kuchepa kwa mulingo wa HbA_1c) ndikuwonjezereka kwa chiwerengero cha odwala omwe ali ndi kuchepa kwa HbA_1c zinali pafupifupi 0.6-0.7% (poyerekeza ndi gulu la odwala lomwe limangolandira metformin yokha).
Odwala omwe amalandila vildagliptin ndi metformin, kusintha kwakukulu pa kulemera kwamunthu poyerekeza ndi koyambirira sikunawonedwe. Masabata 24 atayamba chithandizo, m'magulu a odwala omwe amalandila vildagliptin osakanikirana ndi metformin, kuchepa kwa magazi a systolic ndi diastolic kumadziwika poyerekeza ndi boma loyamba.

Zolemba zosangalatsa

Momwe mungasankhire analog yoyenera
Mu pharmacology, mankhwala nthawi zambiri amagawidwa m'magulumagulu ndi ma analogi. Kapangidwe kazofananira kameneka kamaphatikizira amodzi kapena angapo amomwe omwewo omwe ali ndi mphamvu yothandizira thupi. Ndi ma analogi amatanthauza mankhwala okhala ndi zinthu zosiyanasiyana zogwira ntchito, koma zochizira matenda omwewo.

Kusiyana pakati pa matenda a ma virus ndi bakiteriya
Matenda opatsirana amayambitsidwa ndi ma virus, mabakiteriya, bowa ndi protozoa. Njira ya matenda oyambitsidwa ndi ma virus ndi ma bacteria nthawi zambiri imakhala yofanana. Komabe, kusiyanitsa chomwe chimayambitsa matendawa kumatanthauza kusankha njira yoyenera yomwe ingathandize kuthana ndi vuto lakudzuka ndipo sizingavulaze mwana.

Matalala ndi omwe amayambitsa chimfine
Anthu ena amadziwa vuto lomwe mwana nthawi zambiri amakhala nalo kwa chimfine. Makolo amamutengera kwa madotolo, kukamuyeza mayeso, kugwiritsa ntchito mankhwala osokoneza bongo, ndipo monga chotulukapo chake, mwana amalembetsa kale ndi dotolo wa ana monga nthawi zambiri amadwala. Zoyambitsa zenizeni za kupuma pafupipafupi sizidziwika.

Urology: mankhwalawa a chlamydial urethritis
Chlamydial urethritis nthawi zambiri imapezeka pochita urologist. Amayamba chifukwa cha majeremusi a Chlamidia trachomatis, omwe ali ndi mphamvu ya mabakiteriya komanso mavairasi, omwe nthawi zambiri amafunikira njira yothandizira antibacterial. Imatha kuyambitsa kutupa kosakhudzana ndi urethra mwa amuna ndi akazi.